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PreprintCC BYChemRxiv

Copper-Catalyzed Asymmetric Remote ε-Arylation/Cyclization of Yne-Indole Esters with 5-Aminopyrazoles toward Polycyclic Fused Seven-Membered Azaheterocycles

  • Jiaqi Pu1,2
  • Huanshi Wang1,2
  • Yongsheng Li1,2
  • Shi-Wu Li1,2
  1. 1School of Chemistry and Chemical Engineering/State Key Laboratory Incubation Base for Green Processing of Chemical Engineering
  2. 2Shihezi University
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Abstract

Chiral Cu-catalyzed asymmetric remote ε-arylation/cyclization of yne-indole esters with 5-aminopyrazoles is reported to construct polycyclic fused seven-membered azaheterocycles. After systematic screening of copper sources, chiral ligands, bases and temperature protocols, the optimized CuCl2/L12/DABCO system delivers products in good yields and high enantioselectivities. This transformation exhibits broad substrate compatibility, and steric/electronic effects on stereocontrol are discussed.

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Cite

BibTeXRIS
BibTeX
@misc{pu2026coppercatalyzed,
  title = {{Copper-Catalyzed Asymmetric Remote ε-Arylation/Cyclization of Yne-Indole Esters with 5-Aminopyrazoles toward Polycyclic Fused Seven-Membered Azaheterocycles}},
  author = {Jiaqi Pu and Huanshi Wang and Yongsheng Li and Shi-Wu Li},
  howpublished = {ChemRxiv},
  year = {2026},
  month = oct,
  doi = {10.26434/chemrxiv.15010872/v1},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15010872/v1},
  note = {CC BY},
}
RIS
TY  - UNPB
TI  - Copper-Catalyzed Asymmetric Remote ε-Arylation/Cyclization of Yne-Indole Esters with 5-Aminopyrazoles toward Polycyclic Fused Seven-Membered Azaheterocycles
AU  - Jiaqi Pu
AU  - Huanshi Wang
AU  - Yongsheng Li
AU  - Shi-Wu Li
PY  - 2026
DA  - 2026/10/22
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15010872/v1
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15010872/v1
AB  - Chiral Cu-catalyzed asymmetric remote ε-arylation/cyclization of yne-indole esters with 5-aminopyrazoles is reported to construct polycyclic fused seven-membered azaheterocycles. After systematic screening of copper sources, chiral ligands, bases and temperature protocols, the optimized CuCl2/L12/DABCO system delivers products in good yields and high enantioselectivities. This transformation exhibits broad substrate compatibility, and steric/electronic effects on stereocontrol are discussed.
ER  -